The technology of producing liposomes is fairly mature. Indeed, various nutritional supplements have been formulated in conjunction with liposomes to provide for improved ways of delivering effective doses of the nutritional supplements. Many nutritional supplements may be degraded when taken orally so that their delivery is not be therapeutically effective, encapsulating nutritional supplements with one or more phospholipids to form liposomes provides a measure of protection for the nutritional supplements and may enhance their therapeutic effect. Other capsule and tablet forms of protecting nutritional supplements exist, but when the capsules or tablets disintegrate in the digestive system, the nutritional supplements may not be as well received and delivered to target organs as are encapsulated liposome nutritional supplements combinations. These combinations may be in liquid or aerosol forms too depending on the best desired method of introducing such pharmaceutically active ingredients.
Furthermore, such active pharmaceutical ingredients may also enter the bodily system by passing through skin, and thus enter the systemic circulation, where in time targeted organs may benefit from yet another way of introducing active pharmaceutical ingredients. As is understood in the art skin is generally considered to be fairly impermeable to water. However, under appropriate conditions, as is understood in the art, some pharmaceutically active ingredients actually are able to penetrate the skin and enter into muscles tissues and the blood stream to relieve conditions such as arthritis and even muscle soreness due to overuse of such tissue. Appropriate exercise and appropriate foods and beverages have also been considered to be important components of maintaining good health in immune compromised individuals. Indeed, even when an individual's health is not poor, their immune system may be under attack at all times. Thus a healthy life style plus appropriate liposome nutritional supplements combinations comprising pharmaceutically active ingredients may be highly desirable to continue to remain in good overall health.
It has proven to be difficult to provide stable forms of Iiposome encapsulated nutritional supplements because the technology of making stable liposomes with long term stability is experimentally challenging. Often, the encapsulated nutritional supplements fall out of the Iiposome components and therefore are no longer encapsulated. Storage conditions must be rigorously controlled. Additionally, attempts to improve the stability of such Iiposome encapsulated nutritional supplement combinations have often proven to be specific to the types of nutritional supplements to be delivered and requires considerable formulating expertise.
Consequently, a need exists for improved products and methods for delivering an effective quantity of one or more nutritional supplements (or pharmaceutically active ingredients), wherein the one or more nutritional supplements reach their targeted location prior to any significant degradation. Of course, any appropriate Iiposome delivery pharmacokinetic method may also provide improved products and methods for targeting appropriate locations of the immune system too.
The enteral route of administration is one of the most common routes of administration for pharmaceutical compounds, and food or nutritional supplements. However, not all substances ingested through the enteral route are equally metabolized, and a lot of these substances are heavily metabolized in the gastrointestinal tract. This effect is commonly referred to the first-pass effect (also known as first-pass metabolism or presystemic metabolism). First-pass effect causes the concentration of a drug to be greatly reduced before it reaches the systemic circulation. It is the fraction of lost drug during the process of absorption which is generally related to the liver and gut wall. Notable drugs that experience a significant first-pass effect are imipramine, morphine, propranolol, buprenorphine, diazepam, midazolam, demerol, cimetidine, and lidocaine.
After a drug is swallowed, it is absorbed by the digestive system and enters the hepatic portal system. It is carried through the portal vein into the liver before it reaches the rest of the body. The liver metabolizes many drugs, sometimes to such an extent that only a small amount of active drug emerges from the liver to the rest of the circulatory system. This first pass through the liver thus greatly reduces the bioavailability of the drug. Alternative routes of administration like suppository, intravenous, intramuscular, inhalational aerosol and sublingual avoid the first-pass effect because they allow drugs to be absorbed directly into the systemic circulation.
Therefore, there is a need for formulations for the transmucosal delivery of active ingredients directly into systemic circulation. Furthermore, there is a need for processes for the preparation of formulation for the transmucosal delivery of active ingredients into the systemic circulation.